Herbert Binch
Schering-Plough
12 Papers
287 Citations
Herbert Binch is an academic researcher from Schering-Plough. The author has contributed to research in topics: Muscarinic acetylcholine receptor & Muscarinic acetylcholine receptor M2. The author has an hindex of 11, co-authored 12 publications.
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Papers
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.
Yuguang Wang,Samuel Chackalamannil,Zhiyong Hu,John W. Clader,William J. Greenlee,William Billard,Herbert Binch,Gordon Crosby,Vilma Ruperto,Ruth A. Duffy,Robert D. McQuade,Jean E. Lachowicz +11 more
TL;DR: A series of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes showed pronounced enhancement of brain acetylcholine release after oral administration in the rat microdialysis assay.
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Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.
William J. Greenlee,John W. Clader,Theodros Asberom,Stuart W. McCombie,Jennifer Ford,Henry Guzik,Joseph A. Kozlowski,Shengjian Li,C Liu,Derek B. Lowe,Vice Susan F,H Zhao,Gouwei Zhou,William Billard,Herbert Binch,R Crosby,Ruth A. Duffy,Jean E. Lachowicz,Vicki L. Coffin,Robert W. Watkins,Vilma Ruperto,Catherine D. Strader,Lisa A. Taylor,Kathleen Cox +23 more
TL;DR: Exploration of a series of piperidinylpiperidines has yielded the potent and selective M2 antagonist SCH-217443, which has excellent bioavailability in rats and dogs and shows activity in a rat model of cognition.
69
Facilitation of acetylcholine release and improvement in cognition by a selective M2 muscarinic antagonist, SCH 72788.
Jean E. Lachowicz,Ruth A. Duffy,Vilma Ruperto,Joseph A. Kozlowski,Guowei Zhou,John W. Clader,William Billard,Herbert Binch,Gordon Crosby,Mary Cohen-Williams,Catherine D. Strader,Victoria Coffin +11 more
TL;DR: SCH 72788 is a functional M2 antagonist that competitively inhibits the ability of the agonist oxotremorine-M to inhibit adenylyl cyclase activity, and suggests that M2 receptor antagonists may be useful for treating the cognitive decline observed in AD and other dementias.
37
Substituted 2-(R)-Methyl piperazines as muscarinic M2 selective ligands
Joseph A. Kozlowski,Guowei Zhou,Jayaram R. Tagat,Sue Ing Lin,Stuart W. McCombie,Vilma Ruperto,Ruth A. Duffy,Robert A McQuade,Gordon Crosby,Lisa A. Taylor,William Billard,Herbert Binch,Jean E. Lachowicz +12 more
TL;DR: In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration, and a novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described.
21
Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity.
John W. Clader,William Billard,Herbert Binch,Lian-Yong Chen,Gordon Crosby,Ruth A. Duffy,Jennifer Ford,Joseph A. Kozlowski,Jean E. Lachowicz,Shengjian Li,Charles Liu,Stuart W. McCombie,Vice Susan F,Gowei Zhou,William J. Greenlee +14 more
TL;DR: Anthranilamide analogues such as 23 are potent and highly selective muscarinic M2 antagonists that also show good oral bioavailability and in vivo activity.
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